amg319 and Inflammation

amg319 has been researched along with Inflammation* in 1 studies

Other Studies

1 other study(ies) available for amg319 and Inflammation

Article	Year
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. Journal of medicinal chemistry, 2015, Jan-08, Volume: 58, Issue:1 The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification of 1 (AMG319), a compound with an IC50 of 16 nM in a human whole blood assay (HWB), excellent selectivity over a large panel of protein kinases, and a high level of in vivo efficacy as measured by two rodent disease models of inflammation. Topics: Adenosine; Animals; Autoimmune Diseases; Cells, Cultured; Class I Phosphatidylinositol 3-Kinases; Crystallography, X-Ray; Disease Models, Animal; Drug Discovery; Female; Humans; Inflammation; Mice, Inbred BALB C; Mice, Transgenic; Models, Chemical; Models, Molecular; Molecular Structure; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Quinolines; Rats, Inbred Lew; Sf9 Cells; Structure-Activity Relationship	2015

Article

Year

Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.

Journal of medicinal chemistry, 2015, Jan-08, Volume: 58, Issue:1

The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification of 1 (AMG319), a compound with an IC50 of 16 nM in a human whole blood assay (HWB), excellent selectivity over a large panel of protein kinases, and a high level of in vivo efficacy as measured by two rodent disease models of inflammation.

Topics: Adenosine; Animals; Autoimmune Diseases; Cells, Cultured; Class I Phosphatidylinositol 3-Kinases; Crystallography, X-Ray; Disease Models, Animal; Drug Discovery; Female; Humans; Inflammation; Mice, Inbred BALB C; Mice, Transgenic; Models, Chemical; Models, Molecular; Molecular Structure; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Quinolines; Rats, Inbred Lew; Sf9 Cells; Structure-Activity Relationship

2015